Universidad Peruana Cayetano Heredia

MEFAS, a hybrid of artesunate-mefloquine active against asexual stages of Plasmodium vivax in field isolates, inhibits malaria transmission

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dc.contributor.author Penna-Coutinho, J.
dc.contributor.author da Silva Araújo, M.
dc.contributor.author Campos Aguiar, A.C.
dc.contributor.author Sá, P.M.
dc.contributor.author Rios, C.T.
dc.contributor.author Medeiros, J.F.
dc.contributor.author Pereira, D.B.
dc.contributor.author Boechat, N.
dc.contributor.author Krettli, A.U.
dc.date.accessioned 2021-12-12T20:24:58Z
dc.date.available 2021-12-12T20:24:58Z
dc.date.issued 2021
dc.identifier.uri https://hdl.handle.net/20.500.12866/10282
dc.description.abstract Human malaria continues to be a public health problem and an important cause of morbidity and mortality in the world. Malaria control is achieved through both individual protection against mosquito bites and drug treatment, which is hampered by the spread of Plasmodium falciparum resistance to most antimalarials, including artemisinin derivatives. One of the key pharmacological strategies for controlling malaria is to block transmission of the parasites to their mosquito vectors. Following this rational, MEFAS, a synthetic hybrid salt derived from artesunate (AS) and mefloquine has been previously reported for its activity against asexual P. falciparum parasites in vitro, in addition to a pronounced reduction in the viability of mature gametocytes. Herein, MEFAS was tested against asexual forms of Plasmodium vivax and for its ability to block malaria transmission in Anopheles darlingi mosquitoes in a membrane feeding assay using P. vivax field isolates. MEFAS demonstrated high potency, with a IC50 of 6.5 nM against asexual forms of P. vivax. At 50 μM, MEFAS completely blocked oocyst formation in mosquitoes, regardless of the oocyst number in the control group. At lower doses, MEFAS reduced oocyst prevalence by greater than 20%. At equivalent doses, AS irregularly reduced oocyst formation and caused only slight inhibition of mosquito infections. These results highlight the potential of MEFAS as a novel transmission-blocking molecule, as well as its high blood schizonticidal activity against P. vivax and P. falciparum field isolates, representing a starting point for further development of a new drug with dual antimalarial activity en_US
dc.language.iso eng
dc.publisher Elsevier
dc.relation.ispartofseries International Journal for Parasitology: Drugs and Drug Resistance
dc.rights info:eu-repo/semantics/restrictedAccess
dc.rights.uri https://creativecommons.org/licenses/by-nc-nd/4.0/deed.es
dc.subject Antimalarial en_US
dc.subject Drug resistant en_US
dc.subject New drugs en_US
dc.subject Plasmodium falciparum en_US
dc.subject Plasmodium vivax en_US
dc.subject Transmission blocking en_US
dc.title MEFAS, a hybrid of artesunate-mefloquine active against asexual stages of Plasmodium vivax in field isolates, inhibits malaria transmission en_US
dc.type info:eu-repo/semantics/article
dc.identifier.doi https://doi.org/10.1016/j.ijpddr.2021.09.003
dc.relation.issn 2211-3207


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